| Literature DB >> 15115383 |
Ruengwit Kitbunnadaj1, Obbe P Zuiderveld, Bernard Christophe, Saskia Hulscher, Wiro M P B Menge, Edith Gelens, Erwin Snip, Remko A Bakker, Sylvain Celanire, Michel Gillard, Patrice Talaga, Henk Timmerman, Rob Leurs.
Abstract
In this study, the piperidine ring of immepip and its analogues was replaced by a rigid heterocyclic pyridine ring. Many compounds in the series exhibit high affinity and agonist activity at the human histamine H(3) receptor. Particularly, the 4-pyridinyl analogue of immepip (1c, immethridine) is identified as a novel potent and highly selective histamine H(3) receptor agonist (pK(i) = 9.07, pEC(50) = 9.74) with a 300-fold selectivity over the closely related H(4) receptor.Entities:
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Year: 2004 PMID： 15115383 DOI： 10.1021/jm049932u
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446